PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs; K_i = 26 nM for the rat receptor).¹ It has negligible activity against α1β1γδ and α3β4 nAChRs as well as a panel of monoamine, muscarinic, glutamate, and GABA receptors, except 5-HT₃ (K_i = 930 nM).¹ PNU 282987 evokes whole-cell currents from cultured rat hippocampal neurons and enhances GABAergic synaptic activity when applied to hippocampal slices.²

≥98%